2i3z
From Proteopedia
(New page: 200px<br /><applet load="2i3z" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i3z, resolution 2.900Å" /> '''rat DPP-IV with xan...) |
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| - | [[Image:2i3z.jpg|left|200px]]<br /><applet load="2i3z" size=" | + | [[Image:2i3z.jpg|left|200px]]<br /><applet load="2i3z" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2i3z, resolution 2.900Å" /> | caption="2i3z, resolution 2.900Å" /> | ||
'''rat DPP-IV with xanthine mimetic inhibitor #7'''<br /> | '''rat DPP-IV with xanthine mimetic inhibitor #7'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused | + | A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines. |
==About this Structure== | ==About this Structure== | ||
| - | 2I3Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with LIR as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http:// | + | 2I3Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=LIR:'>LIR</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2I3Z OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Ballaron, S | + | [[Category: Ballaron, S J.]] |
[[Category: Basha, F.]] | [[Category: Basha, F.]] | ||
[[Category: Kurukulasuriya, R.]] | [[Category: Kurukulasuriya, R.]] | ||
[[Category: Lai, C.]] | [[Category: Lai, C.]] | ||
| - | [[Category: Longenecker, K | + | [[Category: Longenecker, K L.]] |
| - | [[Category: Lubben, T | + | [[Category: Lubben, T W.]] |
| - | [[Category: Rohde, J | + | [[Category: Rohde, J J.]] |
| - | [[Category: Sham, H | + | [[Category: Sham, H L.]] |
| - | [[Category: Stewart, K | + | [[Category: Stewart, K D.]] |
| - | [[Category: Szczepankiewicz, B | + | [[Category: Szczepankiewicz, B G]] |
| - | [[Category: VonGeldern, T | + | [[Category: VonGeldern, T W.]] |
[[Category: Winn, M.]] | [[Category: Winn, M.]] | ||
[[Category: LIR]] | [[Category: LIR]] | ||
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[[Category: peptidase]] | [[Category: peptidase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:48:50 2008'' |
Revision as of 15:48, 21 February 2008
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rat DPP-IV with xanthine mimetic inhibitor #7
Overview
A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.
About this Structure
2I3Z is a Single protein structure of sequence from Rattus norvegicus with as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors., Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW, Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. Epub 2006 Sep 28. PMID:17010607
Page seeded by OCA on Thu Feb 21 17:48:50 2008
Categories: Dipeptidyl-peptidase IV | Rattus norvegicus | Single protein | Ballaron, S J. | Basha, F. | Kurukulasuriya, R. | Lai, C. | Longenecker, K L. | Lubben, T W. | Rohde, J J. | Sham, H L. | Stewart, K D. | Szczepankiewicz, B G | VonGeldern, T W. | Winn, M. | LIR | Enzyme | Inhibitor | Peptidase
